Synthesis of 6-amino-6-deoxyhyaluronan as an intermediate for conjugation with carboxylate-containing compounds: application to hyaluronan-camptothecin conjugates.
A novel methodology for making drug conjugates using hyaluronan as a carrier was developed. This strategy involves a completely regioselective two-step synthesis of 6-amino-6-deoxyhyaluronan, which is then easily functionalized with drugs through a suitable linker. The case of hyaluronan-camptothecin conjugates is described, making use of a simple succinate linker. The antitumor activity of new hyaluronan derivatives prepared is at present under evaluation.
Norbedo
Stefano
S
Eurand S.p.A., Area Science Park, Padriciano 99, 34012 Trieste, Italy. stefano.norbedo@eurand.com
Dinon
Francesca
F
Bergamin
Massimo
M
Bosi
Susanna
S
Aroulmoji
Vincent
V
Khan
Riaz
R
Murano
Erminio
E
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry*; D002166:Camptothecin / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry*; D006820:Hyaluronic Acid / Q000737:chemistry*; D015394:Molecular Structure; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D006820:Hyaluronic Acid; D002166:Camptothecin